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重要文件

T0202

Sigma-Aldrich

Tocainide 盐酸盐

≥98% (HPLC), solid

同義詞:

2-Amino-N-(2,6-dimethylphenyl)propanamide 盐酸盐

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About This Item

經驗公式(希爾表示法):
C11H16N2O · HCl
CAS號碼:
分子量::
228.72
EC號碼:
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77
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品質等級

化驗

≥98% (HPLC)

形狀

solid

儲存條件

desiccated
under inert gas

顏色

white

溶解度

DMSO: >20 mg/mL
H2O: ≥5 mg/mL

起源

AstraZeneca

儲存溫度

2-8°C

SMILES 字串

Cl[H].CC(N)C(=O)Nc1c(C)cccc1C

InChI

1S/C11H16N2O.ClH/c1-7-5-4-6-8(2)10(7)13-11(14)9(3)12;/h4-6,9H,12H2,1-3H3,(H,13,14);1H

InChI 密鑰

AMZACPWEJDQXGW-UHFFFAOYSA-N

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應用

Tocainide hydrochloride may be used in cell signaling studies.

生化/生理作用

Tocainide hydrochloride is a primary amine analog of lidocaine (lignocaine), used for the treatment of tinnitus.[1] It blocks the sodium channels in the pain-producing foci in the nerve membranes and renders an analgesic effect in trigeminal neuralgia.[2]
Tocainide hydrochloride is a sodium channel blocker; Class IB antiarrhythmic.

特點和優勢

This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Tocainide is voltage-dependent and use-dependent sodium channel blocker (class IB type antiarrhythmic); Ki = 115 μM in blockade of inactivated-state sodium channels; IC50 = 985μM in blockade of Na+ currents at a holding potential (HP) of -140 mV; IC50 = 254 μM in blockade of Na+ currents at HP -70 mV; IC50 = 523 μM in blockade of Na+ currents at tonic block (-100 mV); IC50 = 248 μM for use-dependent block at 10 Hz.

象形圖

Exclamation mark

訊號詞

Warning

危險聲明

危險分類

Acute Tox. 4 Oral

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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V Challapalli et al.
The Cochrane database of systematic reviews, (4)(4), CD003345-CD003345 (2005-10-20)
Lidocaine, mexiletine, tocainide, and flecainide are local anesthetics which give an analgesic effect when administered orally or parenterally. Early reports described the use of intravenous lidocaine or procaine to relieve cancer and postoperative pain (Keats 1951; Gilbert 1951; De Clive-Lowe
[Na channel myotonia].
H Nemoto et al.
Ryoikibetsu shokogun shirizu, (35)(35), 140-143 (2001-09-15)
P Lindström et al.
Pain, 28(1), 45-50 (1987-01-01)
Tocainide is a derivative of lidocaine with anti-arrhythmic action and, unlike lidocaine, can be used for oral treatment. Tocainide was alternatively with carbamazepine given to 12 patients with trigeminal neuralgia in a double-blind cross-over study for 2 weeks. The analgesic
Annamaria De Luca et al.
Molecular pharmacology, 64(4), 932-945 (2003-09-23)
Newly synthesized tocainide analogs were tested for their state-dependent affinity and use-dependent behavior on sodium currents (INa) of adult skeletal muscle fibers by means of the Vaseline-gap voltage clamp method. The drugs had the pharmacophore amino group constrained in position
Hassan Y Aboul-Enein et al.
Journal of biochemical and biophysical methods, 54(1-3), 407-413 (2003-01-25)
Enantiomeric resolution of thyroxine and tocainide was achieved on a (+)-(18-crown-6)-2,3,11,12-tetracarboxylic acid column. The mobile phases were methanol/water (4:1, v/v) and methanol/water containing 5 mM sulfuric acid (4:1, v/v) for tocainide and thyroxine respectively. The flow rate was 0.5 ml/min.

文章

Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.

电压门控钠通道存在于大多数可兴奋细胞膜中,在产生动作电位方面起着重要作用。

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